Department of Pharmaceutical Chemistry, University Institute of Pharmaceutical Sciences and Research, Baba Farid University of Health Sciences, Faridkot, Punjab, India.
Department of Pharmaceutical Chemistry and Analysis, ISF College of Pharmacy, GT Road, Moga, Punjab, India.
Mini Rev Med Chem. 2021;21(13):1770-1795. doi: 10.2174/1389557521999210101224058.
A sizeable proportion of currently marketed drugs come from heterocycles. The heterocyclic moiety 5-pyrazolone is well known five-membered ring containing nitrogen. Derivatives of this wonder nucleus have exhibited activities as diverse as antimicrobial, anti-inflammatory, analgesic, antidepressant, anticonvulsant, antidiabetic, antihyperlipidemic, antiviral, antitubercular, antioxidant, anticancer and antiviral, including action against severe acute respiratory syndrome (SARS) or 3C protease inhibitor. A number of drugs based on this motif have already made it to the market. Standard texts and literature on medicinal chemistry cite different approaches for the synthesis of 5- pyrazolones. The present review provides an insight view to 5-pyrazolone synthesis, their biological profile and structure-activity relationship studies.
相当一部分目前市场上的药物来自杂环。杂环部分 5-吡唑酮是一种众所周知的含氮五元环。该神奇核的衍生物表现出多种多样的活性，如抗菌、抗炎、镇痛、抗抑郁、抗惊厥、抗糖尿病、抗高血脂、抗病毒、抗结核、抗氧化、抗癌和抗病毒，包括针对严重急性呼吸系统综合症（SARS）或 3C 蛋白酶抑制剂的作用。许多基于这种主题的药物已经上市。药物化学的标准文本和文献引用了合成 5-吡唑酮的不同方法。本综述提供了对 5-吡唑酮合成、生物特征和构效关系研究的深入了解。
